Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier was written by Receveur, Jean-Marie;Murray, Anthony;Linget, Jean-Michel;Norregaard, Pia K.;Cooper, Martin;Bjurling, Emelie;Nielsen, Peter Aadal;Hoegberg, Thomas. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile This article mentions the following:
A series of amides, amidines and amidoximes have been made from the corresponding nitrile compounds, to provide potent antagonists and inverse agonists for the CB1 receptor with considerably lower lipophilicity, higher polar surface area and improved plasma/brain ratios compared to the centrally acting rimonabant. Extensive investigations of ADME and in vivo pharmacol. properties led to selection of the amide series and specifically the 4-(4-fluorophenyl)piperidin-4-ol derivative D4. A clear improvement in the peripheral profile over rimonabant was seen, although some contribution of central effect on the pronounced weight reduction in obese mice cannot be ruled out. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile).
6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics